Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC 50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (K d =0.1 nM).

BIRB 796 is a high affinity and selective p38 kinase inhibitor (K d = 50-100 pM). Exhibits no significant inhibition on a panel of related kinases. Inhibits LPS-induced TNF α production in human PBMCs and whole blood (IC 50 values are 21 and 960 nM, respectively).

BIRB-796 (also known as doramapimod) is one of the most potent compounds that targets a diaryl urea class allosteric binding site, indirectly competes with the binding of adenosine 5′-triphosphate (ATP), which is a novel mechanism in the inhibition of p38 and binds to p38 MAPK with high affinity. 15 BIRB-796 has been continuously studied over ...

2005年5月20日 · The compound BIRB796 inhibits the stress-activated protein kinases p38alpha and p38beta and is undergoing clinical trials for the treatment of inflammatory diseases. Here we report that BIRB796 also inhibits the activity and the activation of SAPK3/p38gamma.

BIRB 796，又称为BIRB-796、Doramapimod，是一种高效的p38 MAPK抑制剂 (Kd=0.1 nM) ，在LPS刺激的THP-1细胞中BIRB 796可以抑制TNF α释放 (IC 50 =18 nM) 。另外，BIRB 796抑制所有的p38 MAPK亚型和c-Jun N末端激酶(JNK)亚型。

BIRB-796 is a highly potent inhibitor of p38 MAPK (Kd = 0.1 nM) that blocks TNFα release in LPS-stimulated THP-1 cells (IC₅₀ = 18 nM) (Pargellis et al.). At 10 μM, BIRB-796 can also inhibit JNK2α2 in vitro, but at lower concentrations BIRB-796 inhibits p38 MAPK without affecting phosphorylation of JNK substrates (Bain et al.; Kuma et al.).

Doramapimod GMP (BIRB 796 GMP) is an orally active inhibitor for p38 MAPK, with IC 50 s of 38, 65, 200 and 520 nM, for p38α, p38β, p38γ, p38δ. Doramapimod exhibits cytotoxicity and antitumor activity against multiple myeloma, synergizes with multidrug resistance protein 1 (ABCB1) and aurora kinase inhibitor VX680, promoting their antitumor ...

birb 796是作用于人类p38 mapk的最有效和分离最慢的抑制剂之一。 BIRB 796 有效抑制c-Raf-1和Jnk2α2，IC50分别为1.4和0.1nM。 高浓度BIRB796也抑制SAPK3/p38γ的活性和激活。

BIRB-796 inhibits the stress-activated p38 mitogen-activated protein kinase (MAPK), which plays a critical role in regulating the production of proinflammatory cytokines such as tumor necrosis factor (TNF) and interleukin 1 (IL-1).

2019年12月26日 · BIRB 796 (p38 MAPK抑制剂)是一种高效的p38α抑制剂，IC50为4 nM，也抑制B-Raf和Abl，IC50分别为83 nM和14.6μM。 由于其在T细胞增殖和细胞因子产生中的作用，通常与炎症相关。